• From an historical perspective ligands for GPCRs

  2022-11-18

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, U 46619 or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were rap

• Therefore the rational design of target

  2022-11-18

  

  Therefore, the rational design of target compounds is based on the hybrid of attractive phenotypic bis-indole (5, Fig. 1) and sulfonamide moieties, in which the indole core might anticipate in hydrophobic interaction, and the functionality of sulfonamide group may involve in H-bonding with the site

• br Materials and methods br Results br Discussion I

  2022-11-18

  

  Materials and methods Results Discussion I/R injury is characterized by myocardial damage triggered by the ischemic insult followed by reperfusion injury. While the primary insult depends mainly on the severity and duration of blood flow restriction and the breakdown of ATP-dependent (+)-MK

• br Obstructing SNARE zippering Sharma

  2022-11-18

  

  Obstructing SNARE “zippering” Sharma et al. demonstrated for the first time that in the postmortem AD brains, the level of SNARE complex formation, which is necessary for driving synaptic vesicle fusion at the presynaptic active zone, is significantly reduced [123]. In the absence of changes in e

• The major phase trial NCT enrolled participants with mild

  2022-11-18

  

  The major phase 2 trial (NCT01343966) enrolled 431 participants with mild to moderate AD who received either low-dose SC crenezumab 300 mg or placebo biweekly (n = 184) or high-dose intravenous crenezumab 15 mg/kg or placebo every 4 weeks (n = 247) for 68 weeks 38, 40. No significant treatment benef

• Clofazimine AMP activated protein kinase AMPK is composed of

  2022-11-18

  

  AMP-activated protein kinase (AMPK) is composed of α-, β-, and γ-subunits [17,18]. Phosphorylation of α-subunit at Thr-172 residue is essential for AMPK activation [17,18]. The serine/threonine kinase coordinates metabolic pathways in response to energy supply and demand [17,18]. Studies have shown

• Introduction Aldose reductase ALR is the first enzyme

  2022-11-18

  

  Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr

• Application of the broad acting HTR antagonist methiothepin

  2022-11-18

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• br Introduction In myasthenia gravis MG autoantibodies again

  2022-11-18

  

  Introduction In myasthenia gravis (MG), autoantibodies against the native AChR conformation cause loss of AChR at the neuromuscular junction and fatigable muscle weakness (Newsom-Davis et al., 1993). The AChR is a pentameric transmembrane protein, with two splice forms of the α-subunit, P3A− and

• The combination of Aurora kinase inhibitors with standard

  2022-11-17

  

  The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the

• Here we report discovery of

  2022-11-17

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of Resiniferatoxin sale bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interact

• Because R gene is positively regulated by

  2022-11-17

  

  Because 5α-R2 gene is positively regulated by T and in the prostate gland (Torres et al., 2003), and our BPA-treated rats showed decreased circulating T and probably intraprostatic androgen levels, it might be responsible for the decrease of 5α-R2 expression. However, in a previous work using castra

• br Introduction Endothelial progenitor cells EPCs present a

  2022-11-17

  

  Introduction Endothelial progenitor cells (EPCs) present a class of blood cells with an ability to form new blood vessels relying on pre-existing vessels, which contribute to postnatal angiogenesis [1], [2]. A wide range of studies have demonstrated that EPCs play a critical role in angiogenesis

• We further conducted stratified analyses to

  2022-11-17

  

  We further conducted stratified analyses to observe changes in enzyme levels across the periods by subgroups. Fig. 1 shows the changes in GPx levels by subgroups of age, sex, and smoking status. In all participants, GPx levels decreased when air pollution levels declined but increased after the Olym

• e3 ligases The rescue of the behavioral deficit was associat

  2022-11-17

  

  The rescue of the behavioral deficit was associated with a significant reduction in the levels of both soluble and insoluble Aβ peptides and their deposition in the e3 ligases of the same animals. In search for the mechanism behind the reduced amyloidosis, we assessed APP metabolism. Confirming pre

7852 records 367/524 page Previous Next First page 上5页 366367368369370 下5页 Last page